Evaluation of gyrase B as a drug target in Mycobacterium tuberculosis | Zendy

Sidharth Chopra | Zendy; Kiminori Matsuyama | Zendy; Thuy Tran | Zendy; Jeremiah P. Malerich | Zendy; B Wan | Zendy; Scott G. Franzblau | Zendy; Shichun Lun | Zendy; Haiyan Guo | Zendy; Mariama C. Maiga | Zendy; William R. Bishai | Zendy; Peter B. Madrid | Zendy

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Evaluation of gyrase B as a drug target in Mycobacterium tuberculosis

Author(s) -

Sidharth Chopra,

Kiminori Matsuyama,

Thuy Tran,

Jeremiah P. Malerich,

B Wan,

Scott G. Franzblau,

Shichun Lun,

Haiyan Guo,

Mariama C. Maiga,

William R. Bishai,

Peter B. Madrid

Publication year - 2011

Publication title -

journal of antimicrobial chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.124

H-Index - 194

eISSN - 1460-2091

pISSN - 0305-7453

DOI - 10.1093/jac/dkr449

Subject(s) - dna gyrase , heterotetramer , mycobacterium tuberculosis , tuberculosis , medicine , antibiotics , pharmacology , drug resistance , drug , protein subunit , microbiology and biotechnology , biology , genetics , escherichia coli , pathology , gene

New classes of drugs are needed to treat tuberculosis (TB) in order to combat the emergence of resistance to existing agents and shorten the duration of therapy. Targeting DNA gyrase is a clinically validated therapeutic approach using fluoroquinolone antibiotics to target the gyrase subunit A (GyrA) of the heterotetramer. Increasing resistance to fluoroquinolones has driven interest in targeting the gyrase subunit B (GyrB), which has not been targeted for TB. The biological activities of two potent small-molecule inhibitors of GyrB have been characterized to validate its targeting as a therapeutic strategy for treating TB.

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